Activity of Repository Sulfones Against Mycobacterium leprae In Mice.

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Abstract
Prompted by the sensitivity of Mycobacterium leprae to very low levels of 4,4[image]-diaminodiphenylsulfone (DDS), 7 discrete repository sulf ones were tested against M. leprae in mice, and all were found completely suppressive when injected at 2-month intervals. DDS was inactive when given at 2-month intervals, partially suppressive at 1-month intervals, and completely suppressive at half-month intervals. The repository sulfone 4,4[image] -diacetyldiamino-diphenylsulfone was titrated in mice against M. leprae. The least dose giving nearly complete suppression was 6 mg/kg/2 months. Cycloguanil pamoate, a repository triazine antimalarial, was inactive in a dose of 400 mg/kg/2 months. Further tests of the sensitivity of M. leprae to DDS were carried out by feeding the drug in the diet. Two strains were completely inhibited by 0.0001%: the same 2 and 2 other strains were insensitive to 0.00001%. Innovations in the current administration regimen of sulfones to leprosy patients were suggested by the efficacy of lower blood levels of DDS as achieved by bi-monthly injections of repository forms.